Three new scientific disciplines show the highest promise of fulfilling the need for increased predictability and for lowering the overall attrition rate of the drug discovery process. (1) Functional Genomics was invented to generate new innovative molecular targets. (2) Combinatorial Chemistry provides increasingly efficient ways to generate molecular diversity with which to probe the targets. (3) High-throughput screening (HTS) plafforms provide efficiency and quality in finding potential lead compounds. High throughput screening within most pharmaceutical companies currently involves performing several million assays per year. Meanwhile, HTS has become a discrete discipline assimilating biochemistry, biophysics and cell/molecular biology combined with detection/liquid handling technologies and automation processes. With all the phantastic oportunities these new scientific disciplines offer, it became already clear, that the time consuming process in functional genomics is the identification of the physiological function of a new protein. Whereas combinatorial chemistry approaches help to synthesize a multifold of compounds during the time needed for classical synthesis, it is known now that between 5 and 10 times the number of assays are needed to identify hit compounds from screens. The challenge the community of applied science is currently faced with, is to fully exploit the advantages of (1) and (2) in a timely manor by speeding up the process of synthesis, protein function identification and screening. The current invention opens a new possibility for integrating the advantages of combinatorial chemistry and genomics with HTS by providing the efficiency needed for screening compounds directly on the solid support. Target macromolecules of even unknown functionality can be tested for their direct binding affinity to compounds of interest. The new fluorescent chemistry, generically described as AlDA-chemistry in the following, is suitable also to screening assays in homogeneous solution, either by direct application of the compounds conjugated to the AlDA chemistry or by cleavage of the AlDA conjugates from the solid support by well known chemical or photophysical means. After the release of the AlDA conjugated "binder" identified in a solid-phase screening technology, the affinity to the macromolecule of interest can be determined by conventional ensemble averaging fluorescence spectroscopic techniques in assay volumes used in microtiter plates. In addition, single molecule spectroscopic techniques performed in microliter volumes and applied in so called nanocarriers can be used.